Structure-activity studies on benzhydrol-containing nipecotic acid and guvacine derivatives as potent, orally-active inhibitors of GABA uptake

…, SJ Lobbestael, D Nugiel, DR Mayhugh…

Index: Pavia, Michael R.; Lobbestael, Sandra J.; Nugiel, David; Mayhugh, Daniel R.; Gregor, Vlad E.; et al. Journal of Medicinal Chemistry, 1992 , vol. 35, # 22 p. 4238 - 4248

Full Text: HTML

Citation Number: 34

Abstract

The introduction of lipophilic groups onto the ring nitrogen of nipecotic acid and guvacine, two known GABA uptake inhibitors, afforded potent, orally-active anticonvulsant drugs. A series of compounds is reported which explores the structure-activity relationships (SAR) in this series. Among the areas explored: side-chain SAR (aromatic-, heterocyclic-, and tricyclic- containing side chains) and modifications to the tetrahydropyridine ring. The benzhydrol ...